Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Robert P. Compton"'
Autor:
Jeffrey L. Hirsch, Robert H. Keith, Loreen Stillwell, Pamela De Ciechi, Jian Zhang, Ravi G. Kurumbail, Richard M. Leimgruber, Shaun R. Selness, Huey S. Shieh, Stephen J. Mnich, Yan Zhang, Barry L. Burnette, Michael Hepperle, Robert P. Compton, Raj Devraj, Gail Jungbluth, Win Naing, Joseph B. Monahan, Joseph Portanova, Gary D. Anderson, Heidi R. Hope
Publikováno v:
Pharmacology. 84:42-60
SD0006 is a diarylpyrazole that was prepared as an inhibitor of p38 kinase-alpha (p38alpha). In vitro, SD0006 was selective for p38alpha kinase over 50 other kinases screened (including p38gamma and p38delta with modest selectivity over p38beta). Cry
Autor:
Joseph Portanova, Robert P. Compton, Shaukat H. Rangwala, Jeffrey L. Hirsch, Lori J. Christine, Joseph B. Monahan, Walter G. Smith
Publikováno v:
Cytokine. 7:775-783
Interleukin 5 (IL-5) has been implicated as a causal mediator in the development of pulmonary eosinophilia and airway hyperreactivity in human asthma. Supportive evidence for a pathogenic role of IL-5 in this disease has been provided by guinea pig m
Autor:
Gabriel Mbalaviele, Rajesh V. Devraj, Elizabeth G. Webb, Jeffrey L. Hirsch, Heidi R. Hope, Matthew J. Saabye, Dean Messing, Jian Zhang, Joseph B. Monahan, Shaun R. Selness, John F. Schindler, Loreen Stillwell, Barry L. Burnette, Gary D. Anderson, Robert P. Compton, Xiong Li, Robert H. Keith
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 331(3)
Signal transduction through the p38 mitogen-activated protein (MAP) kinase pathway is central to the transcriptional and translational control of cytokine and inflammatory mediator production. p38 MAP kinase inhibition hence constitutes a promising t
Autor:
Jennifer M. Williams, Li Xing, Ravi G. Kurumbail, Devadas Balekudru, Jeffrey L. Hirsch, Alan G. Benson, Heidi R. Hope, Roderick A. Stegeman, Zara Walden, Joseph B. Monahan, Shaun R. Selness, Rajesh V. Devraj, Richard M. Broadus, Huey S. Shieh, John K. Walker, Robert P. Compton, John F. Schindler
Publikováno v:
Biochemistry. 48(27)
PH-797804 is a diarylpyridinone inhibitor of p38alpha mitogen-activated protein (MAP) kinase derived from a racemic mixture as the more potent atropisomer (aS), first proposed by molecular modeling and subsequently confirmed by experiments. On the ba
Autor:
Xiong Li, Jacqueline E. Day, James R. Kiefer, Wei Huang, John I. Trujillo, Robin A. Weinberg, Li Xing, Karl J. Mathis, Kuniko K. Kretzmer, Beverley A. Reitz, Nicole Caspers, Lori Christine, Robert P. Compton, Roderick A. Stegeman, Atli Thorarensen, Ann D. Wrightstone
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(3)
The inhibition of PKC-zeta has been proposed to be a potential drug target for immune and inflammatory diseases. A series of 2-(6-phenyl-1H indazol-3-yl)-1H-benzo[d]imidazoles with initial high crossover to CDK-2 has been optimized to afford potent a
Publikováno v:
European Journal of Pharmacology: Molecular Pharmacology. 189:373-379
This study describes a new structural class of compounds which interact at the N-methyl-D-aspartate (NMDA) receptor-associated glycine recognition site. These E-gamma-substituted vinylglycine derivatives were active in displacing [3H]glycine binding
Autor:
Randall K. Rader, William F. Hood, Thomas H. Lanthorn, Yehiel Gaoni, Gerald B. Watson, Robert P. Compton, Joseph B. Monahan
Publikováno v:
European Journal of Pharmacology. 182:397-404
Cis- and trans-2,4-methanoglutamate were compared with L-glutamate as acidic amino acid ligands. Cis-2,4-methanoglutamate had a Ki of 0.052 microM against N-methyl-D-aspartate (NMDA)-specific L-[3H]glutamate binding compared with 0.050 microM for L-g
Autor:
Joseph B. Monahan, J. P. Snyder, Alexis A. Cordi, Benedetto Natalini, Roberto Pellicciari, Robert P. Compton, William F. Hood
Publikováno v:
Neuroscience Letters. 112:328-332
The 4 configurational isomers of d -3,4-cyclopropylglutamate ( d -CGA) have been synthesized and analyzed for their interactions as excitatory amino acid recognition sites. Additionally, functional assessment of the action of these compounds at the N
Publikováno v:
Journal of Neurochemistry. 54:1040-1046
In synaptic plasma membranes from rat forebrain, the potencies of glycine recognition site agonists and antagonists for modulating [3H]1-[1-(2-thienyl)cyclohexyl]piperidine ([3H]TCP) binding and for displacing strychnine-insensitive [3H]glycine bindi
Autor:
Ashok S. Naraian, Gunnar J. Hanson, Huey-Sheng Shieh, Richard Weier, Jennifer L. Pawlitz, William C. Stallings, Robert J. Mourey, Joseph B. Monahan, Lifeng Geng, Ravi G. Kurumbail, Jennifer M. Williams, Robert P. Compton, Matthew J. Graneto, Michael L. Vazquez, Koszyk Francis, Rajesh V. Devraj, Xiangdong D. Xu, Gary D. Anderson, Stephen J. Mnich, Michael A. Stealey
Publikováno v:
Journal of medicinal chemistry. 50(23)
A series of pyrazole inhibitors of p38 mitogen-activated protein (MAP) kinase were designed using a binding model based on the crystal structure of 1 (SC-102) bound to p38 enzyme. New chemistry using dithietanes was developed to assemble nitrogen-lin